An efficient protocol has been developed for the preparation of a series of new 3,4-diaryl-1H-pyrazoles, potential pharmacological and agricultural targets, by the reaction of hydrazine hydrate with different natural isoflavones or their derivatives. The target compounds were obtained in good-toexcellent yields (80 -95%; Table 2) under fairly mild reaction conditions (808) Introduction. (¼ 5,7-dihydroxy-6,4'-dimethoxyisoflavone) is an effective antidiabetic [23]. However, it is necessary to modify the structure of natural isoflavones to increase their biological activities and generally poor solubilities.Recently, we reported the synthesis of several new water-soluble isoflavones [24]. In order to enhance their biological activity and to develop more-powerful new drugs, we herein report the high-throughput synthesis of a series of new 3,4-diarylpyrazoles by means of a one-pot procedure based on the reaction of hydrazine with natural isoflavones.
An orthogonally protected hypusine reagent was developed for solid-phase synthesis of hypusinated peptides using the Fmoc/t-Bu protection strategy. The reagent was synthesized in an overall yield of 27% after seven steps from Cbz-Lys-OBzl and (R)-3-hydroxypyrrolidin-2-one. The side-chain protecting groups (Boc and t-Bu) are fully compatible with standard Fmoc chemistry and can be readily removed during the peptide cleavage step. The utility of the reagent was demonstrated by solid-phase synthesis of hypusinated peptides.
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